10040-88-7Relevant academic research and scientific papers
Evaluation of α-hydroxycinnamic acids as pyruvate carboxylase inhibitors
Burkett, Daniel J.,Wyatt, Brittney N.,Mews, Mallory,Bautista, Anson,Engel, Ryan,Dockendorff, Chris,Donaldson, William A.,St. Maurice, Martin
, p. 4041 - 4047 (2019/08/26)
Through a structure-based drug design project (SBDD), potent small molecule inhibitors of pyruvate carboxylase (PC) have been discovered. A series of α-keto acids (7) and α-hydroxycinnamic acids (8) were prepared and evaluated for inhibition of PC in two assays. The two most potent inhibitors were 3,3′-(1,4-phenylene)bis[2-hydroxy-2-propenoic acid] (8u) and 2-hydroxy-3-(quinoline-2-yl)propenoic acid (8v) with IC50 values of 3.0 ± 1.0 μM and 4.3 ± 1.5 μM respectively. Compound 8v is a competitive inhibitor with respect to pyruvate (Ki = 0.74 μM) and a mixed-type inhibitor with respect to ATP, indicating that it targets the unique carboxyltransferase (CT) domain of PC. Furthermore, compound 8v does not significantly inhibit human carbonic anhydrase II, matrix metalloproteinase-2, malate dehydrogenase or lactate dehydrogenase.
Bioisosteric modification of known fucosidase inhibitors to discover a novel inhibitor of α-l-fucosidase
Bathula, Chandramohan,Ghosh, Shreemoyee,Hati, Santanu,Tripathy, Sayantan,Singh, Shailja,Chakrabarti, Saikat,Sen, Subhabrata
, p. 3563 - 3572 (2017/01/25)
Bioisosteric modification of known fucosidase inhibitors A and B, resulted in three new types of molecules, 4b, 5c and 6a (belonging to furopyridinedione, thiohydantoin and hydantoin chemotypes) that could potentially bind to α-l-fucosidase (bovine kidney
SHIKIMATE PATHWAY INHIBITORS AND THE USE THEREOF
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Paragraph 0041;0042, (2015/05/26)
The present invention relates to methods of inhibiting shikimate pathway, comprising administering to a subject a pharmaceutically acceptable composition comprising a compound having a formula: or pharmaceutically acceptable salts thereof. The present invention also provides a synergistic antibacterial composition containing compound
Expedient base-mediated desulfitative dimethylamination, oxidation, or etherification of 2-(Methylsulfanyl)-3,5-dihydro-4 H -imidazol-4-one scaffolds
Khan, Shahnawaz,Tyagi, Vikas,Mahar, Rohit,Bajpai, Vikas,Kumar, Brijesh,Chauhan, Prem M.S.
, p. 2405 - 2412 (2013/09/23)
The dimethylamino functionality is generally introduced onto the 3,5-dihydro-4H-imidazol-4-one skeleton by treatment of a halogenated derivative with low-boiling dimethylamine at a high temperature and pressure. The corresponding aliphatic ethers are usua
Process for the production of 5-arylidene hydantoins (B)
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, (2008/06/13)
5-Arylidene hydantoins are produced by condensation of an aromatic aldehyde with hydantoin in the presence of at least one ammonium salt of an aliphatic or aromatic carboxylic acid. The desired 5-arylidene hydantoins are obtained in high yields.
Antiviral 5-(substituted benzal) hydantoins
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, (2008/06/13)
Therapeutic compositions containing a compound of the formula: STR1 wherein: R1, R2, and R3 are each hydrogen, hydroxy, alkoxyf 1 to 4 carbon atoms, acyloxy of 1 to 4 carbon atoms, halo, or nitro, or R2 and Rsu
